Anticonvulsant and anxiolytic-like potential of the essential oil from the Ocimum basilicum Linn leaves and its major constituent estragole on adult zebrafish (Danio rerio).

The Ocimum species present active compounds with the potential to develop drugs for treating chronic disease conditions, such as anxiety and seizures. The present study aims to investigate the anticonvulsant and anxiolytic-like effect of the essential oil from O. basilicum Linn (OEFOb) leaves and its major constituent estragole (ES) in vivo on adult zebrafish (aZF) and in silico. The aZF were treated with OEFOb or ES or vehicle and submitted to the tests of toxicity, open-field, anxiety, and convulsion and validated the interactions of the estragole on the involvement of GABAergic and serotonergic receptors by molecular docking assay. The results showed that the oral administration of OEFOb and ES did not have a toxic effect on the aZF and showed anxiolytic-like effects with the involvement of GABAA, 5-HT1, 5-HT2A/2C and 5-HT3A/3B as well on anxiety induced by alcohol withdrawal. The OEFOb and ES showed anticonvulsant potential attenuating the seizures induced by pentylenetetrazole (PTZ) by modulation of the GABAA system. Both anxiolytic and anticonvulsant effects were corroborated by the potential of the interaction of ES by in silico assay. These study samples demonstrate the pharmacological evidence and potential for using these compounds to develop new anxiolytic and anticonvulsant drugs.

Leishmanicidal and immunomodulatory activity of Terminalia catappa in Leishmania amazonensisin vitro infection.

Leishmaniases are infectious-parasitic diseases that impact public health around the world. Antileishmanial drugs presented toxicity and increase in parasitic resistance. Studies with natural products show an alternative to this effect, and several metabolites have demonstrated potential in the treatment of various diseases. Terminalia catappa is a plant species with promising pharmaceutical properties. The objective of this work was to evaluate the therapeutic potential of extracts and fractions of T. catappa on Leishmania amazonensis and investigate the immunomodulatory mechanisms associated with its action. In anti-Leishmania assays, the ethyl acetate fraction exhibited activity against promastigotes (IC50 86.07 ± 1.09 µg/mL) and low cytotoxicity (CC50 517.70 ± 1.68 µg/mL). The ethyl acetate fraction also inhibited the intracellular parasite (IC50 25.74 ± 1.08 µg/mL) with a selectivity index of 20.11. Treatment with T. catappa ethyl acetate fraction did not alter nitrite production by peritoneal macrophages stimulated with L. amazonensis, although there was a decrease in unstimulated macrophages treated at 50 µg/mL (p = 0.0048). The T. catappa ethyl acetate fraction at 100 µg/mL increased TNF-α levels (p = 0.0238) and downregulated HO-1 (p = 0.0030) and ferritin (p = 0.0002) gene expression in L. amazonensis-stimulated macrophages. Additionally, the total flavonoid and ellagic acid content for ethyl acetate fraction was 13.41 ± 1.86 mg QE/g and 79.25 mg/g, respectively. In conclusion, the T. catappa ethyl acetate fraction showed leishmanicidal activity against different forms of L. amazonensis and displayed immunomodulatory mechanisms, including TNF-α production and expression of pro and antioxidant genes.

Anorectal gonorrhoea and chlamydia among transgender women in Brazil: prevalence and assessment of performance and cost of anorectal infection detection and management approaches.

OBJECTIVES: We aimed to determine the prevalence of anorectal Neisseria gonorrhoeae (NG) and Chlamydia trachomatis (CT) among transgender women in Brazil, and to assess the performance and costs of various approaches for the diagnosis and management of anorectal NG/CT. METHODS: TransOdara was a multicentric, cross-sectional STI prevalence study among 1317 transgender women conducted in five capital cities representing all Brazilian regions. Participants aged >18 years were recruited using respondent-driven sampling (RDS), completed an interviewer-led questionnaire, offered an optional physical examination and given choice between self-collected or provider-collected samples for NG/CT testing. Performance and cost indicators of predetermined management algorithms based on the WHO recommendations for anorectal symptoms were calculated. RESULTS: Screening uptake was high (94.3%) and the estimated prevalence of anorectal NG, CT and NG and/or CT was 9.1%, 8.9% and 15.2%, respectively. Most detected anorectal NG/CT infections were asymptomatic (NG: 87.6%, CT: 88.9%), with a limited number of participants reporting any anorectal symptoms (9.1%). Of those who permitted anal examination, few had clinical signs of infection (13.6%). Sensitivity of the tested algorithms ranged from 1.4% to 5.1% (highest for treatment based on the reported anorectal discharge or ulcer and receptive anal intercourse (RAI) in the past 6 months) and specificity from 98.0% to 99.3% (highest for treatment based on the reported anorectal discharge with clinical confirmation or report of RAI). The estimated cost-per-true case of anorectal NG/CT infection treated varied from lowest providing treatment for anorectal discharge syndrome based on the reported RAI ($2.70-4.28), with algorithms including clinical examinations decreasing cost-effectiveness. CONCLUSIONS: High prevalence of mostly asymptomatic anorectal NG and CT was observed among Brazilian transgender women. Multi-site NG/CT screening should be offered to transgender women. Where diagnostic testing capacity is limited, syndromic management for those presenting with anorectal symptoms is recommended.

Antibacterial activity and anxiolytic-like effect of Ziziphus joazeiro Mart. leaves in adult zebrafish (Danio rerio).

Ziziphus joazeiro Mart. is an endemic plant of the Caatinga that presents a great socioeconomic importance for the Northeast and Semiarid Region of Brazil. In view of this, this study aimed to evaluate the antibacterial activity and anxiolytic-like effects of Ziziphus joazeiro Mart leaves in adult zebrafish (Danio rerio). The characterization of the main classes of metabolites was performed through chemical reactions. The antibacterial and antibiotic potentiating activity was evaluated by broth microdilution assays. The 96 h acute toxicity, open field test and anxiety models test was evaluated in vivo on adult zebrafish. The results obtained in the phytochemical prospection evidenced the presence of flobabenic tannins, leucoanthocyanidins, flavonois, flavonones, catechins, alkaloids, steroids, and triterpenoids. EEFZJ did not show antibacterial activity for all microorganism tested (MIC ≥ 1024 µg/mL), but reduced the concentration required for bacterial growth inhibition in combination with gentamicin and norfloxacin against multidrug-resistant strains of S. aureus (SA10) and E. coli (EC06), exhibiting synergistic effect with these antibiotics (p<0.0001). In the tests in vivo, EEFZJ was found to be nontoxic, performing reduced locomotor activity and demonstrated an anxiolytic-like effect in adult zebrafish via GABAergic and Serotoninergic systems (5-HT1, 5-HT2A/2C and 5-HT3A/3B).

Effect of treatment with carvacrol and aerobic training on cardiovascular function in spontaneously hypertensive rats.

NEW FINDINGS: What is the central question of this study? Can two non-drug therapies, carvacrol and aerobic physical training, together have additive effects on the reduction of cardiovascular risks and control of arterial hypertension? What is the main finding and its importance? The oral use of carvacrol (20 mg/kg/day) can control sustained hypertension in spontaneously hypertensive rats, and when this use is associated with aerobic physical training, there is a more pronounced effect on the reduction of blood pressure values, making these therapies an adjunct option in the drug treatment of hypertension. ABSTRACT: Systemic arterial hypertension is considered the foremost cardiovascular risk factor, and it is important to examine different therapies that help prevent and treat it, especially when associated with other cardiovascular risk factors. In this context, it is known that both carvacrol and aerobic physical training benefit the cardiovascular system. This study investigated the effects of treatment with carvacrol combined with aerobic exercise on hypertensive rats with cardiovascular risk parameters. We used an experimental design with six groups: normotensive control (Wistar rats); hypertensive control (spontaneously hypertensive rats, SHR); positive control rats treated with amlodipine (Aml-20 mg); rats treated with carvacrol (Carv-20 mg); rats trained with exercise (Exer); and rats treated with carvacrol and exercise (ExerCarv). The treatment lasted for 4 weeks, monitoring heart rate and systolic blood pressure (SBP). At the end of the treatment, vascular reactivity tests were performed in addition to biochemical measurements of urea, creatinine, aspartate aminotransferase, alanine aminotransferase, triglycerides, total cholesterol, high density lipoprotein cholesterol, low density lipoprotein cholesterol, very low density lipoprotein cholesterol, atherogenic indexes, relative heart weight and histopathological analysis of cardiac perivascular tissue. Significant reductions in SBP were observed after the training period, with the ExerCarv group showing a greater magnitude of reduction (∆SBP = 88 ± 10.0 mmHg, 42%). This group also experienced reductions in atherogenic indices and improvement in all analysed lipid parameters, with no differences observed in the Exer group. The findings indicated that the interaction between aerobic exercise and carvacrol offers a greater BP reduction. Exercise is particularly effective for controlling biochemical parameters of cardiovascular risk, regardless of carvacrol use.

In vitro acaricidal activity of Crescentia cujete L. fruit pulp against Rhipicephalus microplus.

Cattle tick (Rhipicephalus microplus) is an important constraint on livestock production, particularly in tropical and subtropical areas. Synthetic acaricides are the primary method of control this thick. Resistance of R. microplus to synthetic acaricides has given rise to the need of new scientific investigations on alternative ways to control it. The objective of this work was to conduct a chemical investigation of Crescentia cujete L. fruit pulp and to evaluate the acaricide effect on R. microplus larvae of extracts, fractions, and isolated substances from this species. Crescentia cujete is a Bignoniaceae and it is characteristic of tropical climates. Its most distinctive feature is its fruit, which is spherical and gourd-like, with a hard woody shell and gelatinous pulp. The fruit pulp of C. cujete was extracted with ethanol by maceration yielding an extract and a residue. The extract was partitioned giving an ethyl acetate phase (EAF) that was fractionated by chromatographic procedures yielding cinnamic acid and benzoic acid. The remained botanic material from the ethanol extraction was further and successively extracted with ethyl ether and methanol under reflux. The acaricide effect of all extracts and fractions was evaluated against R. microplus using the larval packet test. The best result was observed for the EAF that caused 100% of mortality when a 10% solution was used and with LC50 of 5.9%. Cinnamic acid was also tested showing 63.0% of mortality with LC50 of 6.6% at the same concentrations and time of the experiment. The data obtained in this study provides information related to the chemical nature and the acaricide activity of the C. cujete epicarp that has not been previously reported. This study shows that the ethyl acetate phase of the ethanol extract of C. cujete fruit pulp is a potential alternative control for R. microplus and its activity is in part associated to cinnamic acid, its major compound.

Anthelmintic activity of Leucaena leucocephala protein extracts on Haemonchus contortus.

The objective of this study was to evaluate the effects of protein extracts obtained from the plant Leucaena leucocephala on the nematode parasite Haemonchus contortus. The seeds, shell and cotyledon of L. leucocephala were separated and their proteins extracted using a sodium phosphate buffer, and named as TE (total seed extract), SE (shell extract) and CE (cotyledon extract). Soluble protein content, protease, protease inhibitory and chitinase activity assays were performed. Exsheathment inhibition of H. contortus larvae were performed at concentrations of 0.6 mg mL-1, and egg hatch assays were conducted at protein concentrations of 0.8, 0.4, 0.2, 0.1 and 0.05 mg mL-1. The effective concentration for 50% hatching inhibition (EC50) was estimated by probit. Different proportions of soluble proteins, protease and chitinase were found in TE and CE. Protease inhibitory activity was detected in all extracts. The EC50 of the CE and TE extracts were 0.48 and 0.33 mg mL-1, respectively. No ovicidal effects on H. contortus were detected in SE extracts, and none of the protein extracts demonstrated larvicidal effects on H. contortus. We therefore conclude that protein extracts of L. leucocephala had a detrimental effect on nematode eggs, which can be correlated with the high protease and chitinase activity of these extracts.

Acaricidal activity of Lippia gracilis essential oil and its major constituents on the tick Rhipicephalus (Boophilus) microplus.

The present study aimed to evaluate the activity of Lippia gracilis Schauer essential oil obtained from different L. gracilis genotypes and their major components, carvacrol and thymol against Rhipicephalus (Boophilus) microplus (cattle tick) larvae and engorged females. The larval test was performed parallel to the adult immersion test for engorged females for four L. gracilis genotypes. Similar tests were further performed for their major compounds carvacrol and thymol. Carvacrol (LC50 of 0.22 and 4.46 mg/mL, to larvae and engorged females, respectively) was more efficient than thymol (LC50 of 3.86 and 5.50 mg/mL, to larvae and engorged females, respectively). The lethal concentrations obtained for the isolated essential oil from genotypes LGRA-201 against larvae (1.31 mg/mL) and LGRA-106 against engorged females (4.66 mg/mL) confirmed the acaricidal activity of L. gracilis essential oil and its effectiveness in controlling the southern cattle tick.

Gonadal and nutritional indexes influencing the reproductive behavior of Prochilodus cearensis (Steindachner, 1911) (Characiformes, Prochilodontidae) in Itans water reservoir, Caicó, Rio Grande do N - DOI: 10.4025/actascibiolsci.v25i2.2027 / Indicadores do desenvolvimento gonadal e nutricional de Prochilodus cearensis (Steindachner, 1911) (Characiformes, Prochilodontidae) no açude Itans/Caicó, Rio Grande do Norte, Brasil - DOI: 10.4025/actascibiolsci.v25i2.2027

The aim of this study was to investigate the influence of gonadal and nutritional index on reproductive behavior of Prochilodus cearensis (Steindachner, 1911) (Characiformes, Prochilodontidae) in Itans water reservoir, Caicó, Rio Grande do Norte. 213 animals were used (160 females and 53 males) and collected from Itans water reservoir during the period from April 1996 to January 1997. The highest Gonadossomatic and Gonadal Index values were obtained for females and males from December to February. The repletion index was similar for males and females. The condition factor (ø) showed the highest value just before reproduction. Data collected suggest that reproductive cycle in this species is not directly related to abiotic factors

Analisaram-se alguns aspectos da reprodução e do estado nutricional de 213 exemplares (160 fêmeas e 53 machos) de Prochilodus cearensis no açude Itans/ Caicó no Estado do Rio Grande do Norte, Brasil, no período de abril de 1996 a janeiro de 1997. As médias dos valores dos índices gônadossomático e gonadal apresentaram-se mais elevadas para fêmeas e machos no mês de janeiro. O índice de repleção foi semelhante entre os sexos. O fator de condição (ø) mostrou-se mais elevado no período que antecede à reprodução. Não foi observada correlação significativa entre os fatores abióticos e o ciclo reprodutivo da espécie. No entanto, a presença de indivíduos com gônadas preparadas para a reprodução no trimestre que antecede ao das chuvas sugere que a desova possa estar condicionada a sua ocorrência